Tags

Type your tag names separated by a space and hit enter

Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans.
Eur J Med Chem. 2015 May 05; 95:514-25.EJ

Abstract

We herein report the synthesis and in vitro antimicrobial evaluation of twenty five novel hybrid derivatives of imidazo [2,1-b]-1,3,4-thiadiazole containing chalcones (5a-o) and Schiff bases (6a-j) against three fungal strains (Candida albicans, Cryptococcus neoformans and Aspergillus niger). Most of the tested compounds displayed substantial anti-fungal activity with MICs ranging between 1.56 and 100 μg/mL. Compounds 5a, 5b and 5n exhibited promising activity against C. neoformans at a MIC 1.56 μg/mL. In addition, compound 5n also demonstrated significant antifungal activity against the clinical isolates of C. neoformans at MIC 3.125 μg/mL. However, moderate activity was observed for these compounds against four bacterial strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and Mycobacterium tuberculosis (H37Rv).

Authors+Show Affiliations

Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa. Electronic address: karpoormath@ukzn.ac.za.Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.Department of Microbiology, National Health Laboratory Services (NHLS), Inkosi Albert Luthuli Central Hospital, Durban, South Africa.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

25847769

Citation

Alwan, Wesam S., et al. "Novel Imidazo[2,1-b]-1,3,4-thiadiazoles as Promising Antifungal Agents Against Clinical Isolate of Cryptococcus Neoformans." European Journal of Medicinal Chemistry, vol. 95, 2015, pp. 514-25.
Alwan WS, Karpoormath R, Palkar MB, et al. Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans. Eur J Med Chem. 2015;95:514-25.
Alwan, W. S., Karpoormath, R., Palkar, M. B., Patel, H. M., Rane, R. A., Shaikh, M. S., Kajee, A., & Mlisana, K. P. (2015). Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans. European Journal of Medicinal Chemistry, 95, 514-25. https://doi.org/10.1016/j.ejmech.2015.03.021
Alwan WS, et al. Novel Imidazo[2,1-b]-1,3,4-thiadiazoles as Promising Antifungal Agents Against Clinical Isolate of Cryptococcus Neoformans. Eur J Med Chem. 2015 May 5;95:514-25. PubMed PMID: 25847769.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans. AU - Alwan,Wesam S, AU - Karpoormath,Rajshekhar, AU - Palkar,Mahesh B, AU - Patel,Harun M, AU - Rane,Rajesh A, AU - Shaikh,Mahamadhanif S, AU - Kajee,Afsana, AU - Mlisana,Koleka P, Y1 - 2015/03/12/ PY - 2014/10/03/received PY - 2015/03/09/revised PY - 2015/03/11/accepted PY - 2015/4/8/entrez PY - 2015/4/8/pubmed PY - 2016/1/9/medline KW - Antifungal activity KW - Chalcones KW - Cryptococcosis KW - Cryptococcus neoformans KW - Imdazo [2,1-b]-1,3,4-thiadiazole KW - Schiff bases SP - 514 EP - 25 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 95 N2 - We herein report the synthesis and in vitro antimicrobial evaluation of twenty five novel hybrid derivatives of imidazo [2,1-b]-1,3,4-thiadiazole containing chalcones (5a-o) and Schiff bases (6a-j) against three fungal strains (Candida albicans, Cryptococcus neoformans and Aspergillus niger). Most of the tested compounds displayed substantial anti-fungal activity with MICs ranging between 1.56 and 100 μg/mL. Compounds 5a, 5b and 5n exhibited promising activity against C. neoformans at a MIC 1.56 μg/mL. In addition, compound 5n also demonstrated significant antifungal activity against the clinical isolates of C. neoformans at MIC 3.125 μg/mL. However, moderate activity was observed for these compounds against four bacterial strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and Mycobacterium tuberculosis (H37Rv). SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/25847769/Novel_imidazo[21_b]_134_thiadiazoles_as_promising_antifungal_agents_against_clinical_isolate_of_Cryptococcus_neoformans_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(15)00188-9 DB - PRIME DP - Unbound Medicine ER -